Compounds > mitozolomide
Page last updated: 2024-12-06

mitozolomide

Description

mitozolomide: RN & structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID71766
CHEMBL ID435951
SCHEMBL ID97695
MeSH IDM0120254

Synonyms (49)

Synonym
{imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide,} 3-(2-chloroethyl)-3,4-dihydro-4-oxo-
3-(2-chloroethyl)-4-oxo-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide
3-(2-chloroethyl)-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetraazine-8-carboxamide
NCI60_003169
ccrg-81080
46241-rp
m&b-39565
8-carbamoyl-3-(2-chloroethyl)imidazo(5,1-d)-1,2,3,5-tetrazin-4(3h)-one
3-(2-chloroethyl)-3,4-dihydro-4-oxoimidazo(5,1-d)-as-tetrazine-8-carboxamide
3-(2-chloroethyl)-3,4-dihydro-4-oxoimidazo(5,1-d)-1,2,3,5-tetrazine-8-carboxamide
m & b 39565
einecs 287-943-3
mitozolamide
mitozolomida [spanish]
brn 3618072
ccrg 81010
imidazo(5,1-d)-1,2,3,5-tetrazine-8-carboxamide, 3-(2-chloroethyl)-3,4-dihydro-4-oxo-
nsc 353451
mitozolomidum [latin]
mitozolomide
nsc-353451
imidazo[5,2,3,5-tetrazine-8-carboxamide, 3-(2-chloroethyl)-3,4-dihydro-4-oxo-
azolastone
85622-95-3
mls003171125 ,
nsc353451
CHEMBL435951
3-(2-chloroethyl)-4-oxoimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide
smr001875033
mitozolomide [inn:ban]
e3u7286v3w ,
mitozolomida
unii-e3u7286v3w
mitozolomidum
FT-0630937
mitozolomide [inn]
SCHEMBL97695
DTXSID40234862
3-(2-chloroethyl)-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetraazine-8-carboxamide #
QXYYYPFGTSJXNS-UHFFFAOYSA-N
imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamide, 3-(2-chloroethyl)-3,4-dihydro-4-oxo-
3-(2-chloroethyl)-3,4-dihydro-4-oxoimidazo[5,1-d]-as-tetrazine-8-carboxamide
8-carbamoyl-3-(2-chloroethyl)-imidazo[5,1-d]-1,2,3,5-tetrazin-4-one
8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3h)-one
Q6881926
3-(2-chloroethyl)-4-oxo-3,4-dihydroimidazo[5,1-d][1,2,3,5]tetrazine-8-carboxamide
3-(2-chloroethyl)-4-oxo-3h,4h-imidazo[4,3-d][1,2,3,5]tetrazine-8-carboxamide
EN300-23093670
Z2044764896

Research Excerpts

Overview

Mitozolomide is a novel antitumour agent showing a broad spectrum of activity against murine tumours. It is currently undergoing Phase I clinical evaluation in the UK.

ExcerptReferenceRelevance
"Mitozolomide is a novel antitumour agent showing a broad spectrum of activity against murine tumours and is currently undergoing Phase I clinical evaluation in the UK. "( Antitumour imidazotetrazines, Part IX. The pharmacokinetics of mitozolomide in mice.
Goddard, C; Slack, JA; Stevens, MF, 1985)		1.95

Toxicity

ExcerptReferenceRelevance
" In comparison with control cells that were transfected with the parent vector, the ATase-expressing clones were considerably more resistant to the toxic effects of the methylating agents N-methyl-N-nitrosourea and methylmethanesulphonate or the chloroethylating agents Mz or taurine chloroethylnitrosourea, but unchanged in their susceptibility to the bis-chloroethylating agent nitrogen mustard."( Transfection of murine multi-potent haemopoietic stem cells with an E. coli DNA alkyltransferase gene confers resistance to the toxic effects of alkylating agents.
Dexter, TM; Jelinek, J; Kleibl, K; Margison, GP, 1988)		0.27
" M&B 39565 and MCTIC were 5- to 6-fold more toxic to VA-13 cells than to IMR-90 cells for drug concentrations which produced a 2-log cell kill, as measured by colony-forming assays."( DNA cross-linking and cytotoxicity in normal and transformed human cells treated in vitro with 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d] -1,2,3,5-tetrazin-4(3H)-one.
Erickson, LC; Gibson, NW; Hickman, JA, 1984)		0.27
"001) to the toxic effects of this drug."( Recombinant adeno-associated virus-mediated expression of O6-alkylguanine-DNA-alkyltransferase protects human epithelial and hematopoietic cells against chloroethylating agent toxicity.
Arrand, JR; Berns, KI; Cortez, N; Fairbairn, LJ; Giraud, C; Longhurst, SJ; Rafferty, JA, 1999)		0.3

Pharmacokinetics

ExcerptReferenceRelevance
" In an attempt to relate dose and pharmacokinetic parameters to toxicity, we measured plasma concentrations of mitozolomide in 14 patients with a range of malignancies."( Relationship between the pharmacokinetics and toxicity of mitozolomide.
Blackledge, GR; Bradley, C; Kaye, SB; Kerr, DJ; Secrett, P; Slack, JA; Stevens, MF, 1990)		0.73
" We have conducted an animal pharmacokinetic study using male BALB/c mice as a pre-requisite to the clinical work."( Antitumour imidazotetrazines, Part IX. The pharmacokinetics of mitozolomide in mice.
Goddard, C; Slack, JA; Stevens, MF, 1985)		0.51

Dosage Studied

ExcerptRelevanceReference
" The major toxicity was myelosuppression which necessitated reduction in the initial dosage from 115 to 90 mg/m2."( Phase II studies of mitozolomide in melanoma, lung and ovarian cancer.
Docherty, V; Dorward, A; Harding, M; Kaye, S; Mackie, R, 1989)		0.6
" MTZ, according to this schedule and dosage does not show significant activity in human squamous cell head and neck cancer."( Phase II study of mitozolomide (M & B 39,565) in head and neck cancer.
Armand, JP; Benahmed, M; Cvitkovic, E; Delgado, FM; Domenge, C; Fontana, X; Herait, P; Recondo, G, 1989)		0.61
"8%, respectively, of those seen when mice were dosed with authentic methylmitozolomide."( Metabolism and murine pharmacokinetics of the 8-(N,N-dimethylcarboxamide) analogue of the experimental antitumor drug mitozolomide (NSC353451).
Gescher, A; Horspool, KR; Lunt, E; Quarterman, CP; Slack, JA; Stevens, MF, 1989)		0.72
" Since high levels of the enzyme confer the efficient repair of DNA alkylation, the chemotherapeutic potential of alkylating chemicals can be maintained either increasing drug dosage or reducing the amount of endogenous MGMT."( The sensitivity of MCF10A breast epithelial cells to alkylating drugs is enhanced by the inhibition of O6-methylguanine-DNA methyltransferase transcription with a synthetic double strand DNA oligonucleotide.
Citti, L; Colombo, MG; Mariani, L; Piccirilli, A; Poliseno, L; Rainaldi, G, 2002)		0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (174)

Assay IDTitleYearJournalArticle
AID120186Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119622Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119612Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124600Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1 -5 T/C = days test animals live/days control animals live x 100; >60/10.41984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100953Antitumor activity was assessed against L1210 tumors in B6D2F1 mouse by inoculation of 10e5 tumor cells through intravenous route and number of Survivors to duration was reported at 40 mg/kg peroral dose; 1/71987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID120170Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on days 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122064Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120169Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID16927Mean rate constant for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(A)-d(T) (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID120177Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID24905Half life for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Centigrade in incubation mixture - d(G)-d(C) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID712167Cytotoxicity against human A2780 cells after 5 days by MTT assay in presence of 10 uM MGMT inactivator Patrin22012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR.
AID100972Antitumor activity was assessed against L1210 tumors in B6D2F1 mouse by inoculation of 10e5 tumor cells through intravenous route and mean death of animals (treated/control) was reported at 20 mg/kg peroral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID122067Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120181Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID24901Half life for the hydrolysis of compound in buffers at pH 6.5, at 37 degrees Celsius in incubation mixture - d(G)-d(C) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID81318In vitro cytotoxicity against human xeroderma pigmentosum fibroblast cells HMGZAT (mer+)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID209692In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 5 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID122066Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124728Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; >60/10.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122046Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 3.12 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119615Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-5 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID16925Mean rate constant for the hydrolysis of compound in buffers at pH 7.4 at 37 degrees Centigrade in incubation mixture - d(A)-d(T) (10:!)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID712168Cytotoxicity against human A2780 cells after 5 days by MTT assay2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR.
AID209551In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 20 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID100946In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 40 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID122063Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122065Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID24906Half life for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(G)-d(C) (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID16923Mean rate constant for the hydrolysis of compound in buffers at pH 6.5, at 37 degrees Celsius in incubation mixture - d(A)-d(T) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119608Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122050Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119606Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID16928Mean rate constant for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(G)-d(C) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119617Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120185Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122047Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122059Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120182Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209544In vitro cytotoxicity against mouse TLX5 lymphoma cells1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119623Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124735Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 15/9.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID28475Hydrolytic parameter (K) was calculated at pH 7.4 in 0.1 M phosphate buffer (25 degrees Celsius)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID209859Antitumor activity was assessed against TLX5 tumors in CBA/CA mouse by inoculation of 2 x 10e5 tumor cells through subcutaneous route and mean death of animals (treated/control) was reported at 5 mg/kg ip dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID124719Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 3.12 mg/kg/day on day 1-9 T/C = days test animals live/days control animals live x 100; 12.1 / 8.21984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID26695Half-life period in 95% ethanol in dark at 28 degrees celsius.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122051Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120173Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-91984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID712166Cytotoxicity against MMR-deficient human A2780/CP70 cells after 5 days by MTT assay in presence of 10 uM MGMT inactivator Patrin22012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR.
AID26697Half-life period in 95% ethanol in diffuse laboratory light at 28 degrees celsius.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120172Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122062Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122068Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124736Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 13.2/10.01984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124731Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; >60/10.01984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100947In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 5 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID124721Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-9 T/C = days test animals live/days control animals live x 100; 11.3/8.21984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209688In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 20 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID16924Mean rate constant for the hydrolysis of compound in buffers at pH 6.5, at 37 degrees Celsius in incubation mixture - d(G)-d(C) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID16926Mean rate constant for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - 5'-GMP/5'-CMP (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID73184In vitro cytotoxicity against human lymphoblastoid cell line (GM892 A)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID120189Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120180Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124724Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-9 T/C = days test animals live/days control animals live x 100; 15.1 / 8.21984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119610Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-9 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124716Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 16/8.11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122052Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119609Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124727Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 16.4/10.01984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122049Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122069Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID766221Ratio of IC50 for human HCT116 cells expressing p53 to IC50 for p53-deficient human HCT116 cells2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Synthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA-methyltransferase, DNA mismatch repair, and p53.
AID124601Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 10.6/8.11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119613Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209983In vitro cytotoxicity against mouse TLX5 lymphoma cells2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID124718Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-9 T/C = days test animals live/days control animals live x 100; >61.1 / 8.21984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119620Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124739Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; >60/10.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119598Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID24902Half life for the hydrolysis of compound in buffers at pH 7.4 at 37 degrees Celsius in incubation mixture - d(A)-d(T) (10:!)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID120188Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124726Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 14.1/8.11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120183Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119603Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on days 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100975Antitumor activity was assessed against L1210 tumors in B6D2F1 mouse by inoculation of 10e5 tumor cells through intravenous route and mean death of animals (treated/control) was reported at 5 mg/kg peroral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID24900Half life for the hydrolysis of compound in buffers at pH 6.5, at 37 degrees Celsius in incubation mixture - d(A)-d(T) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119611Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120165Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124717Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on days 1-5 T/C = days test animals live/days control animals live x 100; >60/10.41984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID16929Mean rate constant for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(G)-d(C) (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID122056Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120174Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124715Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 11.6/10.41984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124725Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 17.0/10.41984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID27023Half life calculated for hydrolysis in 0.1 M phosphate buffer at 37 degrees Centigrade (pH 7.4)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID120179Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119626Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID712165Cytotoxicity against MMR-deficient human A2780/CP70 cells after 5 days by MTT assay2012ACS medicinal chemistry letters, Dec-13, Volume: 3, Issue:12
Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR.
AID100923In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 20 mg/kg on 7th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID209706Antitumor activity was assessed against TLX5 tumors in CBA/CA mouse by inoculation of 2 x 10e5 tumor cells through subcutaneous route and number of Survivors to duration was reported at 40 mg/kg ip dose; 4/51987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID100944In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 20 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID81319In vitro cytotoxicity against human xeroderma pigmentosum fibroblast cells HMGZip (mer-)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID124714Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; >61.1 / 8.21984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120164Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 3.12 mg/kg/day on day 1-91984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID27022Half life calculated for hydrolysis in 0.1 M phosphate buffer at 25 degrees Celsius (pH 7.4)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID231797Ratio of cytotoxicity against Raji cells to that of GM892 A cells.1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID124732Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; >60/10.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124730Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 16/10.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122055Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124729Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 27/9.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119604Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-9 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119618Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119601Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120190Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122053Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209548In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 10 mg/kg on 5th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID124734Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; >60/10.01984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209690In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 40 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID100969Antitumor activity was assessed against L1210 tumors in B6D2F1 mouse by inoculation of 10e5 tumor cells through intravenous route and mean death of animals (treated/control) was reported at 10 mg/kg peroral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID119600Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-9 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122058Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209856Antitumor activity was assessed against TLX5 tumors in CBA/CA mouse by inoculation of 2 x 10e5 tumor cells through subcutaneous route and mean death of animals (treated/control) was reported at 40 mg/kg ip dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID28476Hydrolytic parameter (K) was calculated at pH 7.4 in 0.1 M phosphate buffer (37 degrees Celsius)2002Journal of medicinal chemistry, Dec-05, Volume: 45, Issue:25
Antitumor imidazotetrazines. 41. Conjugation of the antitumor agents mitozolomide and temozolomide to peptides and lexitropsins bearing DNA major and minor groove-binding structural motifs.
AID120166Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122070Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID16930Mean rate constant for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(G)-d(T) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID124738Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 17.8/9.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209685In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 10 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID24907Half life for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(G)-d(T) (10:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID26698Half-life period in phosphate buffer at pH 7.4 in the dark at 28 degrees celsius.1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120168Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100943In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 10 mg/kg1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID24903Half life for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Centigrade in incubation mixture - 5'-GMP/5'-CMP (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119624Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-5 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124733Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 38/9.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122048Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120178Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120175Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID165776In vitro cytotoxicity against Raji cell line1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119605Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 3.12 mg/kg/day on day 1-9 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122054Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209557In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 5 mg/kg on 5th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID120184Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119619Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-5 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119602Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 20 mg/kg/day on day 1 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209852Antitumor activity was assessed against TLX5 tumors in CBA/CA mouse by inoculation of 2 x 10e5 tumor cells through subcutaneous route and mean death of animals (treated/control) was reported at 20 mg/kg ip dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID124737Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 30/10.81984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID766223Chemosensitization of human HCT116 cells expressing p53 after 5 days by MTT assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Synthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA-methyltransferase, DNA mismatch repair, and p53.
AID124720Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 40 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; > 60/8.11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100927In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 5 mg/kg on 7th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID119599Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on days 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120171Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 25 mg/kg/day on day 1-91984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122057Compound was evaluated for number of survivors in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120176Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 6.25 mg/kg/day on day 1-91984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124722Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 9.0/8.11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120332Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 11984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID122061Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 60 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119616Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 2.5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124740Compound was tested for MST in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 80 mg/kg/day on day 1 T/C = days test animals live/days control animals live x 100; 7.4 / 10.01984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119614Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 10 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100973Antitumor activity was assessed against L1210 tumors in B6D2F1 mouse by inoculation of 10e5 tumor cells through intravenous route and mean death of animals (treated/control) was reported at 40 mg/kg peroral dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID24904Half life for the hydrolysis of compound in buffers at pH 7.4, at 37 degrees Celsius in incubation mixture - d(A)-d(T) (1:1)1995Journal of medicinal chemistry, Apr-28, Volume: 38, Issue:9
Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
AID119625Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 7.5 mg/kg/day on day 1-5 out of 5 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID120187Compound was evaluated for %T/C in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-51984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209847Antitumor activity was assessed against TLX5 tumors in CBA/CA mouse by inoculation of 2 x 10e5 tumor cells through subcutaneous route and mean death of animals (treated/control) was reported at 10 mg/kg ip dose1987Journal of medicinal chemistry, Feb, Volume: 30, Issue:2
Antitumor imidazotetrazines. 14. Synthesis and antitumor activity of 6- and 8-substituted imidazo[5,1-d]-1,2,3,5-tetrazinones and 8-substituted pyrazolo[5,1-d]-1,2,3,5-tetrazinones.
AID119607Compound was tested for mortality in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-9 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID119621Compound was tested for mortality in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 50 mg/kg/day on day 1-5 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID209556In vivo antitumor activity against the TLX5 lymphoma cell line in mouse species CBA/CA after intraperitoneal administration (inoculum cells-2x10E5,sc) at the dose of 40 mg/kg on 5th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID120167Compound was evaluated for %T/C in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 1-91984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID124723Compound was tested for MST in L1210 leukemia implanted BDF1 mice on day 0 after ip administration of 5 mg/kg/day on day 1-5 T/C = days test animals live/days control animals live x 100; 14.4/10.41984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID100922In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 10 mg/kg on 7th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID100926In vivo antitumor activity against the L1210 leukemia cell line in mouse species B6D2F1 after peroral administration (inoculum cells-10E5,iv) at the dose of 40 mg/kg on 7th day1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Antitumor imidazotetrazines. 20. Preparation of the 8-acid derivative of mitozolomide and its utility in the preparation of active antitumor agents.
AID122060Compound was evaluated for number of survivors in P388 leukemia implanted BDF1 mice on day 0 after ip administration of 12.5 mg/kg/day on day 60 out of 6 mice1984Journal of medicinal chemistry, Feb, Volume: 27, Issue:2
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
AID766222Chemosensitization of p53-deficient human HCT116 cells after 5 days by MTT assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Synthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA-methyltransferase, DNA mismatch repair, and p53.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (75)

TimeframeStudies, This Drug (%)All Drugs %
pre-199040 (53.33)18.7374
1990's25 (33.33)18.2507
2000's6 (8.00)29.6817
2010's4 (5.33)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.05

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index19.05 (24.57)
Research Supply Index4.41 (2.92)
Research Growth Index4.16 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (3.85%)5.53%
Reviews1 (1.28%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other74 (94.87%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
taurine
[no description available]		3.7621amino sulfonic acid;
zwitterion		antioxidant;
Escherichia coli metabolite;
glycine receptor agonist;
human metabolite;
mouse metabolite;
nutrient;
radical scavenger;
Saccharomyces cerevisiae metabolite
ametantrone
ametantrone: RN given refers to parent cpd; structure		1.9710
carmustine
Carmustine: A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed). carmustine : A member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group.		2.8840N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
chlorambucil
Chlorambucil: A nitrogen mustard alkylating agent used as antineoplastic for chronic lymphocytic leukemia, Hodgkin's disease, and others. Although it is less toxic than most other nitrogen mustards, it has been listed as a known carcinogen in the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (Merck Index, 11th ed). chlorambucil : A monocarboxylic acid that is butanoic acid substituted at position 4 by a 4-[bis(2-chloroethyl)amino]phenyl group. A chemotherapy drug that can be used in combination with the antibody obinutuzumab for the treatment of chronic lymphocytic leukemia.		1.9710aromatic amine;
monocarboxylic acid;
nitrogen mustard;
organochlorine compound;
tertiary amino compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
lomustine
[no description available]		3.7620N-nitrosoureas;
organochlorine compound		alkylating agent;
antineoplastic agent
mechlorethamine
nitrogen mustard : Compounds having two beta-haloalkyl groups bound to a nitrogen atom, as in (X-CH2-CH2)2NR.		1.9710nitrogen mustard;
organochlorine compound		alkylating agent
methyl methanesulfonate
[no description available]		1.9710methanesulfonate esteralkylating agent;
apoptosis inducer;
carcinogenic agent;
genotoxin;
mutagen
mitoxantrone
Mitoxantrone: An anthracenedione-derived antineoplastic agent.. mitoxantrone : A dihydroxyanthraquinone that is 1,4-dihydroxy-9,10-anthraquinone which is substituted by 6-hydroxy-1,4-diazahexyl groups at positions 5 and 8.		1.9710dihydroxyanthraquinoneanalgesic;
antineoplastic agent
netropsin
Netropsin: A basic polypeptide isolated from Streptomyces netropsis. It is cytotoxic and its strong, specific binding to A-T areas of DNA is useful to genetics research.		2.0110
o(6)-benzylguanine
O(6)-benzylguanine: a suicide inhibitor of O(6)-methylguanine-DNA methyltransferase activity		2.420
pentobarbital
Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236). pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups.		1.9610barbituratesGABAA receptor agonist
phenobarbital
Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups.		1.9610barbituratesanticonvulsant;
drug allergen;
excitatory amino acid antagonist;
sedative
temozolomide
[no description available]		6.48200imidazotetrazine;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent;
prodrug
thymidine
[no description available]		2.3720pyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
metabolite;
mouse metabolite
uridine
[no description available]		1.9610uridinesdrug metabolite;
fundamental metabolite;
human metabolite
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		2.0110pyrrole;
secondary amine
quinazolines
Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.		2.0510azaarene;
mancude organic heterobicyclic parent;
ortho-fused heteroarene;
quinazolines
aminoimidazole carboxamide
Aminoimidazole Carboxamide: An imidazole derivative which is a metabolite of the antineoplastic agents BIC and DIC. By itself, or as the ribonucleotide, it is used as a condensation agent in the preparation of nucleosides and nucleotides. Compounded with orotic acid, it is used to treat liver diseases.. 5-aminoimidazole-4-carboxamide : An aminoimidazole in which the amino group is at C-5 with a carboxamido group at C-4.		2.3720aminoimidazole;
monocarboxylic acid amide		mouse metabolite
methylnitrosourea
Methylnitrosourea: A nitrosourea compound with alkylating, carcinogenic, and mutagenic properties.. N-methyl-N-nitrosourea : A member of the class of N-nitrosoureas that is urea in which one of the nitrogens is substituted by methyl and nitroso groups.		2.6730N-nitrosoureasalkylating agent;
carcinogenic agent;
mutagen;
teratogenic agent
ethylnitrosourea
Ethylnitrosourea: A nitrosourea compound with alkylating, carcinogenic, and mutagenic properties.. N-ethyl-N-nitrosourea : A member of the class of N-nitrosoureas that is urea in which one of the nitrogens is substituted by ethyl and nitroso groups.		4.2740N-nitrosoureasalkylating agent;
carcinogenic agent;
genotoxin;
mutagen
etoposide
[no description available]		6.9710beta-D-glucoside;
furonaphthodioxole;
organic heterotetracyclic compound		antineoplastic agent;
DNA synthesis inhibitor
elliptinium
elliptinium: synthetic ellipticine deriv; RN given refers to parent cpd; structure given in first source		1.9710carbazoles
n-(2-chloroethyl)-n-nitrosoacetamide
N-(2-chloroethyl)-N-nitrosoacetamide: structure given in first source		3.0610
1-(2-chloroethyl)-3-(2-(dimethylaminosulfonyl)ethyl)-1-nitrosourea
[no description available]		3.7621
cyclodisone
cyclodisone: structure given in first source		1.9710
adenosine
quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit		1.9610adenosines;
purines D-ribonucleoside		analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
o-(6)-methylguanine
O-(6)-methylguanine: structure. 6-O-methylguanine : A methylguanine in which the methyl group is positioned on the oxygen at position 6. Formed in DNA by alkylation of the oxygen atom of guanine, most often by N-nitroso compounds and sometimes due to methylation by other compounds such as endogenous S-adenosylmethionine, it base-pairs to thymine rather than cytidine, causing a G:C to A:T transition in DNA.. methylguanine : A 2-aminopurine that is guanine bearing a single methyl substituent.		2.3820methylguaninemutagen
1-(2-chloroethyl)-1-nitrosourea
[no description available]		4.0430
5-(3-methyl-1-triazeno)imidazole-4-carboxamide
5-(3-methyl-1-triazeno)imidazole-4-carboxamide: structure; RN given refers to parent cpd. MTIC : A monocarboxylic acid amide that is dacarbazine in which one of the methyl groups is replaced by a hydrogen. It is the active metabolite of dacarbazine, and is also produced by spontaneous hydrolysis of temozolomide in the body.		1.9810imidazoles;
monocarboxylic acid amide;
triazene derivative		alkylating agent;
antineoplastic agent
clomesone
clomesone: structure & RN given in first source		5.3740
cyanates
Cyanates: Organic salts of cyanic acid containing the -OCN radical.. cyanates : Salts and esters of cyanic acid, HOC#N; compounds carrying the cyanate functional group -O-C#N.. isocyanates : Organonitrogen compounds that are derivatives of isocyanic acid; compounds containing the isocyanate functional group -N=C=O (as opposed to the cyanate group, -O-C#N).		2.0110
lexitropsin
lexitropsin: structure given in first source; information reading oligopeptide		7.0110
ethazolastone
ethazolastone: structure given in first source		4.4550
beta-lactams
2-azetidinone: structure in first source. azetidin-2-one : An unsubstituted beta-lactam compound.. beta-lactam : A lactam in which the amide bond is contained within a four-membered ring, which includes the amide nitrogen and the carbonyl carbon.		2.0110beta-lactam antibiotic allergen;
beta-lactam
melphalan
Melphalan: An alkylating nitrogen mustard that is used as an antineoplastic in the form of the levo isomer - MELPHALAN, the racemic mixture - MERPHALAN, and the dextro isomer - MEDPHALAN; toxic to bone marrow, but little vesicant action; potential carcinogen.. melphalan : A phenylalanine derivative comprising L-phenylalanine having [bis(2-chloroethyl)amino group at the 4-position on the phenyl ring.		2.0710L-phenylalanine derivative;
nitrogen mustard;
non-proteinogenic L-alpha-amino acid;
organochlorine compound		alkylating agent;
antineoplastic agent;
carcinogenic agent;
drug allergen;
immunosuppressive agent
thioguanine anhydrous
Thioguanine: An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.. tioguanine : A 2-aminopurine that is the 6-thiono derivative of 2-amino-1,9-dihydro-6H-purine. Incorporates into DNA and inhibits synthesis. Used in the treatment of leukaemia.		1.98102-aminopurinesanticoronaviral agent;
antimetabolite;
antineoplastic agent
alpha-chymotrypsin
Chymotrypsin: A serine endopeptidase secreted by the pancreas as its zymogen, CHYMOTRYPSINOGEN and carried in the pancreatic juice to the duodenum where it is activated by TRYPSIN. It selectively cleaves aromatic amino acids on the carboxyl side.		1.9610
ethoglucid
imidazole mustard: inhibitor of purine nucleoside synthesis; minor descriptor (77-84); on-line & Index Medicus search NITROGEN MUSTARD COMPOUNDS (77-84); RN given refers to parent cpd		1.9710
oligonucleotides
[no description available]		2.0110
sparsomycin
Sparsomycin: An antitumor antibiotic produced by Streptomyces sparsogenes. It inhibits protein synthesis in 70S and 80S ribosomal systems.		6.9710
nu 1025
NU 1064: structure in first source		2.0510phenols;
quinazolines		EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor
guanine
[no description available]		5.97802-aminopurines;
oxopurine;
purine nucleobase		algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
dacarbazine
(E)-dacarbazine : A dacarbazine in which the N=N double bond adopts a trans-configuration.		11.47200dacarbazine
methylnitronitrosoguanidine
Methylnitronitrosoguanidine: A nitrosoguanidine derivative with potent mutagenic and carcinogenic properties.. N-methyl-N'-nitro-N-nitrosoguanidine : An N-nitroguanidine compound having nitroso and methyl substituents at the N'-position		1.9610nitroso compoundalkylating agent
ConditionIndicatedRelationship StrengthStudiesTrials
Experimental Leukemia
[description not available]		05.1660
Leukemia L 1210
[description not available]		03.5830
Germinoblastoma
[description not available]		03.9850
Lymphoma
A general term for various neoplastic diseases of the lymphoid tissue.		08.9850
Astrocytoma, Grade IV
[description not available]		02.0510
Glial Cell Tumors
[description not available]		02.0510
Glioblastoma
A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.		02.0510
Glioma
Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)		02.0510
Cancer of Prostate
[description not available]		02.0710
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		02.0710
Breast Cancer
[description not available]		07.6730
Breast Neoplasms
Tumors or cancer of the human BREAST.		02.6730
Carcinoma 256, Walker
A transplantable carcinoma of the rat that originally appeared spontaneously in the mammary gland of a pregnant albino rat, and which now resembles a carcinoma in young transplants and a sarcoma in older transplants. (Stedman, 25th ed)		01.9610
Cell Transformation, Neoplastic
Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.		04.8240
Anaplastic Astrocytoma
[description not available]		01.9810
Benign Neoplasms, Brain
[description not available]		01.9810
Malignant Melanoma
[description not available]		04.8681
Astrocytoma
Neoplasms of the brain and spinal cord derived from glial cells which vary from histologically benign forms to highly anaplastic and malignant tumors. Fibrillary astrocytomas are the most common type and may be classified in order of increasing malignancy (grades I through IV). In the first two decades of life, astrocytomas tend to originate in the cerebellar hemispheres; in adults, they most frequently arise in the cerebrum and frequently undergo malignant transformation. (From Devita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2013-7; Holland et al., Cancer Medicine, 3d ed, p1082)		01.9810
Brain Neoplasms
Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.		01.9810
Melanoma
A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)		04.8681
Cancer of Ovary
[description not available]		03.0750
Ovarian Neoplasms
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.		03.0750
Abnormalities, Autosome
[description not available]		01.9810
Bladder Cancer
[description not available]		02.3820
Cancer of Testis
[description not available]		01.9810
Urinary Bladder Neoplasms
Tumors or cancer of the URINARY BLADDER.		02.3820
Testicular Neoplasms
Tumors or cancer of the TESTIS. Germ cell tumors (GERMINOMA) of the testis constitute 95% of all testicular neoplasms.		01.9810
Sarcoma, Epithelioid
[description not available]		03.7621
Thrombopenia
[description not available]		04.2741
Sarcoma
A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant.		03.7621
Soft Tissue Neoplasms
Neoplasms of whatever cell type or origin, occurring in the extraskeletal connective tissue framework of the body including the organs of locomotion and their various component structures, such as nerves, blood vessels, lymphatics, etc.		03.3611
Thrombocytopenia
A subnormal level of BLOOD PLATELETS.		04.2741
Benign Neoplasms
[description not available]		04.2741
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		04.2741
Bone Cancer
[description not available]		01.9810
Cancer of Lung
[description not available]		03.4780
Cancer of Skin
[description not available]		02.3820
Bone Neoplasms
Tumors or cancer located in bone tissue or specific BONES.		01.9810
Lung Neoplasms
Tumors or cancer of the LUNG.		03.4780
Skin Neoplasms
Tumors or cancer of the SKIN.		02.3820
Carcinoma, Oat Cell
[description not available]		01.9710
Carcinoma, Non-Small Cell Lung
[description not available]		02.3720
Carcinoma, Non-Small-Cell Lung
A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.		02.3720
Carcinoma, Small Cell
An anaplastic, highly malignant, and usually bronchogenic carcinoma composed of small ovoid cells with scanty neoplasm. It is characterized by a dominant, deeply basophilic nucleus, and absent or indistinct nucleoli. (From Stedman, 25th ed; Holland et al., Cancer Medicine, 3d ed, p1286-7)		01.9710
Experimental Mammary Neoplasms
[description not available]		01.9710
Carcinoma, Epidermoid
[description not available]		01.9710
Cancer of Head
[description not available]		01.9710
Local Neoplasm Recurrence
[description not available]		01.9710
Carcinoma, Squamous Cell
A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)		01.9710
Head and Neck Neoplasms
Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651)		01.9710
Leukocytopenia
[description not available]		02.3720
Carcinoma, Transitional Cell
A malignant neoplasm derived from TRANSITIONAL EPITHELIAL CELLS, occurring chiefly in the URINARY BLADDER; URETERS; or RENAL PELVIS.		01.9710
Leukopenia
A decrease in the number of LEUKOCYTES in a blood sample below the normal range (LEUKOCYTE COUNT less than 4000).		02.3720
Metastase
[description not available]		01.9710
Neoplasm Metastasis
The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.		01.9710
Adenocarcinoma Of Kidney
[description not available]		01.9710
Cancer of Kidney
[description not available]		01.9710
Carcinoma, Renal Cell
A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.		01.9710
Kidney Neoplasms
Tumors or cancers of the KIDNEY.		01.9710
Adenocarcinoma, Basal Cell
[description not available]		02.6630
Cancer of Colon
[description not available]		02.8840
Adenocarcinoma
A malignant epithelial tumor with a glandular organization.		02.6630
Colonic Neoplasms
Tumors or cancer of the COLON.		02.8840
Colorectal Cancer
[description not available]		01.9710
Colorectal Neoplasms
Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.		01.9710
Osteogenic Sarcoma
[description not available]		01.9610
Osteosarcoma
A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)		01.9610
Acute Myelogenous Leukemia
[description not available]		01.9710
Leukemia, Myeloid, Acute
Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES.		01.9710
Testicular Diseases
Pathological processes of the TESTIS.		01.9710
Blood Diseases
[description not available]		03.3511
Hematologic Diseases
Disorders of the blood and blood forming tissues.		03.3511
Nausea
An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.		03.3511
Bone Marrow Diseases
Diseases involving the BONE MARROW.		01.9710
Cancer of Liver
[description not available]		01.9710
Lymph Node Metastasis
[description not available]		01.9710
Liver Neoplasms
Tumors or cancer of the LIVER.		01.9710
Cancer of the Uterus
[description not available]		01.9710
Choriocarcinoma
A malignant metastatic form of trophoblastic tumors. Unlike the HYDATIDIFORM MOLE, choriocarcinoma contains no CHORIONIC VILLI but rather sheets of undifferentiated cytotrophoblasts and syncytiotrophoblasts (TROPHOBLASTS). It is characterized by the large amounts of CHORIONIC GONADOTROPIN produced. Tissue origins can be determined by DNA analyses: placental (fetal) origin or non-placental origin (CHORIOCARCINOMA, NON-GESTATIONAL).		06.9710
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		01.9710
Uterine Neoplasms
Tumors or cancer of the UTERUS.		01.9710
Experimental Neoplasms
[description not available]		01.9610
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